Sunitinib Malate

Licensed by Pfizer Catalog No.S1042

Sunitinib Malate Chemical Structure

Molecular Weight(MW): 532.56

Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit.

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In DMSO USD 191 In stock
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USD 147 In stock
USD 447 In stock
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Cited by 42 Publications

12 Customer Reviews

  • PDGF-AA induces Ezh2 expression and proliferation in juvenile islets but not in adult islets. Western immunoblots of indicated islet proteins from 3 week or 9 month-old WT islets 2 days after exposure to PDGF-AA alone, or PDGF-AA plus RTK inhibitors Sunitinib.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck.

    Assessment of effects on human juvenile or adult islets after exposure to PDGF-AA (50 ng/ml) for 2 days, with or without Sunitinib (2 uM) or U0126 (10 uM)co-treatment. Average percentage of BrdU+ insulin+ cells was morphometry from sectioned islets immunostained for insulin (green), glucagon (white) and BrdU (red). n = 3-6 independent experiments.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck.

  • Combinational treatment of kinase inhibitors induces the similar phenotype produced by PP1. All images are lateral view with dorsal to the top and anterior to the left. The combinational treatment of Dasatinib (D) or U0126 (U) with Sunitinib (SU),PTK787 (PTK), or ZM323881 (Z) resulted in the shrinkage of dorsal aorta.

    Cell Res 2011 21, 1080-1087. Sunitinib Malate purchased from Selleck.

    A, Tumor growth curves from the initial sunitinib drug trials, with endpoint set at 1,300 mm3 (mean ± SEM). Measurements began one week after tumor inoculation and on the day sunitinib treatment began. Subsequent experimental endpoints were set on the basis of these growth curves and their intersections with this data are shown. B, Histogram plot showing the distribution of tumor sizes at day 8 of treatment. Sunitinib-treated tumors exceeding 250 mm3 in size were identified as falling into the nonresponsive cohort. Sunitinib treatment significantly retards growth of responsive tumors.

    Cancer Res, 2017, 77(4):1008-1020 . Sunitinib Malate purchased from Selleck.

  • Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading.

    Surgery 2012 152, 1045-50. Sunitinib Malate purchased from Selleck.

    Sunitinib or PD98059 decreases cell proliferation in a dose-dependent manner. H295R and SW13 cells were treated with various concentration of sunitinib or PD98059 for 48 hours as indicated. Treated cells were subjected to the MTS proliferation assay. Similar experiments were repeated 3 times. Histograms represent relative % of OD490 nm absorbance (* P < .05). All data are relative multiples of expression compared with untreated cells. The data are representative of three experiments and are expressed as the mean ?SE.

    Surgery 2012 152, 1045-50. Sunitinib Malate purchased from Selleck.

  • Autophagic activation in sunitinib- and sorafenib- but not AZD6244-treated cells. Medullary thyroid cancer-1.1 (MTC-1.1; A) and TT ( B) cells were treated with dimethyl sulfoxide (DMSO), sunitinib (50 nM), sorafenib (10 nM), AZD6244 (30 nM), or everolimus (20 nM) for 48 hours. Cell lysates were prepared, and light chain 3 (LC3)-I and -II cleaved caspase-3 protein levels were monitored by Western blotting. Reprobing against actin was per formed to ensure equal protein loading. ( C ) MTC-1.1 and TT cells were transiently transfected with autophagy protein 5 (Atg-5) small inter fering RNA. Transfection with scrambled small inter fering RNA was used as a control. After transfection, cells with and without Atg-5 knockdown were exposed to DMSO or 20 nM of everolimus for 48 hours. Cell lysates were pre- pared and LC3-I and -II protein expression levels were monitored by Western blotting. Reprobing against Atg-5 was per formed to monitor Atg-5 knockdown efficiency. Reprobing against actin was per formed to ensure equal protein.

    Surgery 2012 152, 1142-9. Sunitinib Malate purchased from Selleck.

    Autophagy inhibition blocks the antiproliferative effects of sunitinib and sorafenib but not AZD6244. Medullary thyroid cancer–1.1 (MTC-1.1) and TT cells were transfected transiently with scrambled or autophagy protein 5 (Atg-5) small inter fering RNA. After transfection, cells with and without Atg-5 knockdown were exposed to sunitinib (50 nM), sorafenib (10 nM), and AZD6244 (30 nM) for 48 hours. Treated cells were subjected to a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium proliferation assay. Similar experiments were repeated 3 times. Histograms represent the relative percent of OD490 nM absorbance. The asterisk indicates significance versus scrambled small inter fering RNA–treated control ( P < .05). All data are relative multiples of expression compared to untreated cells. The data are representative of 3 experiments and are expressed as the mean ± the standard error.

    Surgery 2012 152, 1142-9. Sunitinib Malate purchased from Selleck.

  • Sunitinib limits the colonial growth of HT-29 by downregulating HIF-1a. (A) The number and size of colonies formed in soft agar. The numbers of small colonies (<50 μm diameter) were not different among conditions of a serial concentration of sunitinib. On the contrary, large colonies (>50 μm diameter) disappeared after incubation with sunitinib. Each point represents the mean and SD from four separate experiments. (B) HIF-1a expression and hypoxia within HT-29 colony. After colonies grew for 4 weeks, HIF-1a and hypoxia were visualized by immunofluoroscence staining. Bar = 20 μm.

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

    2. Sunitinib downregulates HIF-1a. (A) Dose-dependent repression of HIF-1a protein level by sunitinib in HT-29. HT-29 cells were incubated under normoxic (N) or hypoxic (H) conditions in the presence of sunitinib for 24 h. HIF-1a and ARNT proteins in total cell lysates were analyzed by Western blotting. (B) Sunitinib attenuates the hypoxic induction of HIF-1 target genes. RNAs were isolated from HT-29 cells subjected to normoxia (N) or hypoxia (H) in the presence of sunitinib for 16 h. The mRNAs of HIF-1a and its target genes were analyzed by RT-PCR and autoradiography. PGK1 indicates phosphoglycerate kinase 1; PDK1, pyruvate dyhydrogenase kinase 1; CAIX, carbonic anhydrase IX. (C) Sunitinib-induced HIF-1 inhibition. Epo-enhancer and b- galactosidase reporter plasmids were co-transfected into HEK293 cells. After 16 h incubation, luciferase and b-galactosidase activities were measured. *P < .05 versus the hypoxic control.

     

     

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

  • Sunitinib inhibits 50-UTR-dependent translation of HIF-1a. (A) 50 cap-dependent translational activity of HIF-1a. The luciferase reporter plasmid contains the HIF-1a 50-UTR segment between the tk promoter and the luciferase gene. HT-29 cells were co-transfected with the reporter plasmid (8 lg per 100-mm dish) and the b-gal plasmid (4 μg). After 16 h incubation under normoxic or hypoxic conditions with sunitinib, cells were lysed and subjected to luciferase assay. *P < .05 versus the hypoxic control. (B) IRES-dependent translational activity of HIF-1a. The luciferase reporter plasmid contains the HIF-1a 50-UTR segment between the GFP gene and the luciferase gene. HT-29 cells were co-transfected with the reporter plasmid (8 μg) and the b-gal plasmid (4 μg). *P < .05 versus the hypoxic control. (C) Sunitinib inhibits phosphorylation of Akt. After 8 h incubation under hypoxic condition with sunitinib, HT-29 cells were lysed and subjected to Western blotting. (D) Sunitinib suppresses HIF-1a in VHL-null RCC4 cells. VHL (-/-) RCC4 cells were incubated under normoxic conditions sunitinib for 8 h, and HIF-1a in total cell lysates was analyzed by Western blotting.

     

     

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

    Experimental layout for VEGF signaling blocking and LCMV infection in WT mice. Mice received two injections on day 0 and 3 p.i. of Abs as described in Material and Methods, or daily gavage of the VEGFR/PDGFR-inhibitor sunitinib. Inguinal LN volume on day 0 (D0) or day 8 (D8) p.i. after treatment of mice with control Ig or anti-VEGFR2, anti-VEGF-A Abs or sunitinib. Pooled from 1-2 independent experiments with 3-5 mice per treatment. D. Total HEV length on day 0 (D0) or day 8 (D8) p.i. as in C. No significant difference was found in C and D between day 8 control Ig and Ab- or inhibitor-treated values (One-way ANOVA).

    AACR Sunitinib Malate purchased from Selleck.

Purity & Quality Control

Choose Selective PDGFR Inhibitors

Biological Activity

Description Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit.
Targets
Kit [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
2 nM 80 nM
In vitro

Sunitinib also potently inhibits Kit and FLT-3. [1] Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. [2] Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3 NVnQVZdwU2mwYYPlJGF{e2G7 MoCyTY5pcWKrdHnvckBw\iCSRFfGMYlv\HWlZXSgRpJlXSCrbnPvdpBwemG2aX;uJJdqfGhiSVO1NEBw\iByLkCwO{DPxE1? M2q4[|EzPjR4MEG5
3T3 M3PrNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PXeGlvcGmkaYTpc44hd2ZiUHzheIVt\XRvZHXybZZm\CCpcn;3eIgh\mGldH;yJIlv\HWlZXSgN3Q{KGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4xOSEQvF2= MkHYNVI3PDZyMUm=
3T3 M2fH[GZ2dmO2aX;uJGF{e2G7 M{m1dmlvcGmkaYTpc44hd2ZiVnHzZ5Vt[XJiZX7kc5Rp\WyrYXyg[5Jwf3SqIH\hZ5RweiC{ZXPldJRweiC5aYToJGlEPTBib3[gNE4xPSEQvF2= MmTuNVI3PDZyMUm=
3T3 MWXLbY5ie2ViQYPzZZk> MVeyNEBucW5? MoC3SG1UVw>? NID3eGRE\WyudXzhdkBqdmirYnn0bY9vKG:oIG\FS2YhcW6mdXPl[EBpfW2jbjDLSHIheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyNkDPxE1? M2rYOFE3OTZ{MEC4
NIH3T3 Mn3IT4lv[XOnIFHzd4F6 NEjxd3gzOCCvaX6= Ml\wSG1UVw>? Mm\XbY5pcWKrdDDoeY1idiCNRGKgb4lv[XOnIHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOC5yMUig{txO NVqydYlCOTZzNkKwNFg>
A549 NV65SVVzTnWwY4Tpc44hSXO|YYm= MXrEUXNQ MnX0TY5pcWKrdHnvckBw\iClLV3leEBl\XCnbnTlcpQhUEeILXnu[JVk\WRiaIXtZY4hSTV2OTDj[YxtKG2rZ4LheIlwdiC5aYToJGlEPTBib3[gNkDPxE1? M1XOVVE5PDN2MUS1
DU145 M{HWPGZ2dmO2aX;uJGF{e2G7 MUTEUXNQ NX:1b5NLUW6qaXLpeIlwdiCxZjDjMW1mfCCmZYDlcoRmdnRiSFfGMYlv\HWlZXSgbJVu[W5iRGWxOFUh[2WubDDzZ4F1fGW{aX7nJJdqfGhiSVO1NEBw\iBzMDFOwG0> M4Txd|E5PDN2MUS1
KB3-1 M4PhdWN6fG:2b4jpZ{BCe3OjeR?= MnrkO|IhcA>? NUTKS2NDTE2VTx?= MoTFR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVE1oeC2wZXfheIl3\SCNQj2zMVEh[2WubIOge4l1cCCLQ{WwJI9nKDJwMzFOwG0> MXqxPVM6PzN{Mh?=
KBV1 MYnDfZRwfG:6aXOgRZN{[Xl? M1HmflczKGh? MX7EUXNQ M3TqeWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHAu\2y7Y3;wdo91\WmwLXX4dJJme3OrbnegT2JXOSClZXzsd{B4cXSqIFnDOVAhd2ZiND6xJO69VQ>? NWCyVoZPOTl|OUezNlI>
A375 Ml3vR5l1d3SxeHnjJGF{e2G7 MnmzO|IhcA>? M3PRW2ROW09? NYLY[ZJNUUN3ME21MlQh|ryP MonwNVk3PTR2MEi=
RS4-11 M1fhdWZ2dmO2aX;uJGF{e2G7 MV[yJIg> Ml[3TY5pcWKrdHnvckBw\iCITGSzJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFA6QSEQvF2= MYqxPVY2PDRyOB?=
RS4-11 M3fUfWZ2dmO2aX;uJGF{e2G7 M4TX[lIhcA>? NX63UG1XUW6qaXLpeIlwdiCxZjDGUHQ{KEmWRDDteZRidnRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yM{Sg{txO NGTGSGkyQTZ3NESwPC=>
Sf9 NH;TV3JMcW6jc3WgRZN{[Xl? NULqdXJNOzBibXnu Ml3NTY5pcWKrdHnvckBw\iCJU2SteIFo\2WmIG\FS2ZTKGW6cILld5Nm\CC5aYToJGlEPTBib3[gNE4yQDVizszN M2m0VFE6QDV2MEWx
Ba/F3 NYq3bpo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nNVFczKGh? M1K3SmlEPTB;MT6yJO69VQ>? Mnv4NlAyOTdyMES=
BaPTC2 NILkcIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlX1O|IhcA>? NGLoNpFKSzVyPUCuNlIh|ryP NE\uOlkzODFzN{CwOC=>
Sf9 NHW1doRHfW6ldHnvckBCe3OjeR?= NVvjOJl3OSCq MX7EUXNQ Ml63TY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCKaYOteIFo\2WmIGLFWEBmgHC{ZYPz[YQhf2m2aDDJR|UxKG:oIEGuN{DPxE1? M2HVdFIxOTF5MEC0
H4 NU\FUHFSS3m2b4TvfIlkKEG|c3H5 MmfGNVAh|ryP M3LWSnRwgGmlaYT5JIlvKGi3bXHuJGg1KGOnbHzz MnLHNlA{PTB6ME[=
SF-539 M{izVmtqdmG|ZTDBd5NigQ>? NFu1S5k{OzNizszN M2PxclYxKG2rbh?= NVPQOmY1TE2VTx?= M1K4eWlvcGmkaYTpc44hd2ZiUFTHSnJj\XSjIIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNVIvOiEQvF2= M4L0UVIxPDB|N{Cw
U251 NGPidVNMcW6jc3WgRZN{[Xl? MmfXN|M{KM7:TR?= MnjBOlAhdWmw MWjEUXNQ Mnq0TY5pcWKrdHnvckBw\iCYRVfGVlIheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iBzOD65JO69VQ>? MVKyNFQxOzdyMB?=
A431 MVLLbY5ie2ViQYPzZZk> NVfBOGp6UW6qaXLpeIlwdiCxZjDQSGdHWmKndHGg[ZhxemW|c3XkJJdqfGhiSVO1NEBw\iBzMj6yJO69VQ>? Ml\sNlA2PThyN{K=
A431 NFzJWHdMcW6jc3WgRZN{[Xl? Ml;sTY5pcWKrdHnvckBw\iCYRVfGVlIh\XiycnXzd4VlKHerdHigTWM2OCCxZjCxPE46KM7:TR?= NXTCN3RTOjB3NUiwO|I>
HepG2 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV23NkBp M2DhZ2lEPTB;Mz64NUDPxE1? NFrJboozODV5MEWyOi=>
Kasumi-1 NEC3b2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTIXIs4OiCq M33VTWlEPTB;MD6wNVYh|ryP NHPwRmYzODV5MEWyOi=>
RS4-11 NHLTb5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV:3NkBp MX\JR|UxRTFizszN M4DZVVIxPTdyNUK2
THP1 NHnXendIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXJO|IhcA>? M{LYTWlEPTB;MD61JO69VQ>? Ml7ONlA2PzB3Mk[=
Kasumi-1 MXPGeY5kfGmxbjDBd5NigQ>? MWrJcohq[mm2aX;uJI9nKGNvS3n0JIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFE2KM7:TR?= MV:yNFg{OzB|OR?=
A549 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVWxOkBp NFPrOI1CdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzz Mm\mNlE1PTB2NkO=
HL60 NW\B[IJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDxUnIyPiCq MYPBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy| M4[2eVIyPDVyNE[z
HUVEC MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXrXWMyPiCq MoOzTY5pcWKrdHnvckBw\iCYRVfGMYlv\HWlZXSgZ4VtdCCycn;sbYZmemG2aX;uJJdqfGhiSVO1NEBw\iB{Lke1JO69VQ>? MUWyNVQ2ODR4Mx?=
HUVEC M1P5XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWixOkBp NGrZS3lKdmirYnn0bY9vKG:oIHLGS2YucW6mdXPl[EBk\WyuIIDyc4xq\mW{YYTpc44hf2m2aDDJR|UxKG:oIESuNFQh|ryP NVPXNY9xOjF2NUC0OlM>
IM9 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVexOkBp NYHmWIxwSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gTW06KGOnbHzz NIHpW5kzOTR3MES2Ny=>
K562 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPheWkyPiCq NGn0[VNCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzz MXeyNVQ2ODR4Mx?=
MDA-MB-231 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYCxOkBp NIi2fFFCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy| NWfhNnBWOjF2NUC0OlM>
H460 M3;CNGN6fG:2b4jpZ{BCe3OjeR?= NWDUUYl3PzJiaB?= NIT5No5KSzVyPUKuO{DPxE1? MkPTNlE3OjF6OEC=
SMMC7721 M{\hR2N6fG:2b4jpZ{BCe3OjeR?= M2f4XlczKGh? MkLuTWM2OD14LkS3JO69VQ>? Mk\jNlE3OjF6OEC=
WI38 MoXOR5l1d3SxeHnjJGF{e2G7 NGj4TpA4OiCq MmHOTWM2OD16LkW2JO69VQ>? NWqzWJczOjF4MkG4PFA>
HEK293 MUDLbY5ie2ViQYPzZZk> M3LMXlExOCCwTR?= M3;kelEhcA>? MoXt[I9meyCwb4SgbY5pcWKrdDDWSWdHNWmwZIXj[YQh[XW2b4Doc5NxcG:{eXzheIlwdiCxZjD0fZJwe2mwZTCxNVc2KHKnc3nkeYUhd25iVlXHSnIzKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJM> NWPkUJZyOjF6OEWyPFc>
HUVEC NET2fJJHfW6ldHnvckBCe3OjeR?= NFTDTVgyKM7:TR?= NUHaTYpOOjRiaB?= Mnz5RY51cWGwZ3nv[4VvcWNiYXP0bZZqfHliYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hXkWJRj3pcoR2[2WmIHPlcIwhdWmpcnH0bY9v M4rIXVIyQTZ|M{C1
HUVEC NYn2R2MzTnWwY4Tpc44hSXO|YYm= MVWxJO69VQ>? MkPqNUBp M3HpfmlvcGmkaYTpc44hd2ZiRWLLJJBpd3OyaH;yfYxifGmxbjDheEBVcHJ{MEKvWJlzOjB2IHnuJHZGT0Zvc4TpcZVt[XSnZDDIWXZGSw>? M2GxbVIyQTZ|M{C1
HUVEC NITxTZFHfW6ldHnvckBCe3OjeR?= MV2xJO69VQ>? MYCxJIg> MXvJcohq[mm2aX;uJI9nKGWQT2OgdIhwe3Cqb4L5cIF1cW:wIHH0JHNmei1zMUeyJIlvKF[HR1[td5RqdXWuYYTl[EBJXV[HQx?= MX6yNVk3OzNyNR?=
HUVEC Mn\CT4lv[XOnIFHzd4F6 NIHabowyKM7:TR?= MY[xJIg> MWjJcohq[mm2aX;uJI9nKF[HR1\SNkBxcG:|cHjvdplt[XSrb36gZZQhfHm{LUGxO|UhcW5iVlXHSk1{fGmvdXzheIVlKEiXVlXD MVyyNVk3OzNyNR?=
HUVEC MkjuSpVv[3Srb36gRZN{[Xl? M4TjelEh|ryP NGOzcHoyKGh? NVHGbnZi\G:nczDuc5QhcW6qaXLpeEBCU1RicHjvd5Bpd3K7bHH0bY9vKGG2IGPldk01PzNiaX6gWmVITi2|dHnteYxifGWmIFjVWmVE M{XkdlIyQTZ|M{C1
HL60 M4TFd2N6fG:2b4jpZ{BCe3OjeR?= MUm1NEDPxE1? M3PCdlQ5KGh? M4fPbWROW09? MV;JR|UxRTF3LkWg{txO M{Xyc|IzODF7MUi4
K562 NWDJUHpZS3m2b4TvfIlkKEG|c3H5 M2GyZ|UxKM7:TR?= MoXlOFghcA>? M3r1NGROW09? M4nrcWlEPTB;MkGuPUDPxE1? MWmyNlAyQTF6OB?=
PC3 NILOVZhEgXSxdH;4bYMhSXO|YYm= Mo\yOVAh|ryP M3SzW|Q5KGh? NV\SfmpGTE2VTx?= MmLuTWM2OD1{NT6xJO69VQ>? NFfFWoczOjBzOUG4PC=>
SF-539 MVTLbY5ie2ViQYPzZZk> MoTLN|M{KM7:TR?= NHLqTlU3OCCvaX6= M{jyT2lvcGmkaYTpc44hd2ZiUFTHSnJj\XSjIIT5do9{cW6nIHvpcoF{\SCjY4Tpeol1gSCrbjDQSGdHNUKELYP0bY12dGG2ZXSgbJVu[W5iU1[tOVM6KGOnbHzzJJdqfGhiSVO1NEBw\iBzMj6yJO69VQ>? NF\NUIIzOjJyNEe0NS=>
HAEC MmLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;RTlFwOTByIN88US=> NWLFVXI3PzJiaB?= MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiDRVOgZ4VtdHNiZYjwdoV{e2mwZzDWSWdHWiC5aYToJGlEPTBib3[gNE4yKM7:TR?= NGjXfmEzOjR2NE[3PS=>
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EoL-1-cell MoPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLBOmVKSzVyPUGuOlQheE1? MWHTRW5ITVJ?
MV-4-11 Mn;TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTJ5MjDwUS=> MV3TRW5ITVJ?
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CGTH-W-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDNTWM2OD1|MD65OEBvVQ>? MUXTRW5ITVJ?
MONO-MAC-6 NHnvZXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGj5dItKSzVyPUOzMlghdk1? MUDTRW5ITVJ?
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NKM-1 MlHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvlPWhUUUN3ME25PE42OiCwTR?= M4TuXXNCVkeHUh?=
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SIG-M5 M2HRUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\t[4NOUUN3ME2xMlM4ODB7IN88US=> NFvBfG1USU6JRWK=
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A3-KAW MlP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXYO3Q{UUN3ME2xMlYzPTR4IN88US=> NF:2TmpUSU6JRWK=
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EMG-01 MmPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDaZ2U6UUN3ME2xMlg{PTZ|IN88US=> MVzTRW5ITVJ?
TE-11 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPmTWM2OD1zLkizPVg2KM7:TR?= M3HDenNCVkeHUh?=
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NB1 MmTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXOS2RNUUN3ME2xMlk3OTF5IN88US=> NGWwXZBUSU6JRWK=
HAL-01 NGr1SVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;RU2tKSzVyPUKuNFU6PDZizszN MV;TRW5ITVJ?
DEL NFvze45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLH[YZ1UUN3ME2yMlA5PDh{IN88US=> NUexR256W0GQR1XS
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KARPAS-299 M3fuUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDqSlM4UUN3ME2yMlEyOzF|IN88US=> NGDidYdUSU6JRWK=
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RPMI-8402 M1f6UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonOTWM2OD1{LkOzOlE5KM7:TR?= NFHhb4lUSU6JRWK=
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TE-8 NEfUUnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;RTWM2OD1{LkO3NFM5KM7:TR?= MXLTRW5ITVJ?
K052 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXZTWM2OD1{LkSwNlAzKM7:TR?= NWPX[GtKW0GQR1XS
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ML-2 NFO1S3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjLc29KSzVyPUKuOlM2OTJizszN NV;uWldTW0GQR1XS
LAMA-84 MkDIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF62TldKSzVyPUKuOlk2PDVizszN NHz3OWdUSU6JRWK=
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NCI-H82 MlHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnP5TWM2OD15LkO3PFUh|ryP NWTkPFNCW0GQR1XS
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NCI-H209 M3HQOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDUOnFKSzVyPUiuNVE3PTJizszN MWrTRW5ITVJ?
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NCI-H1648 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXuz[FU4UUN3ME25MlE{QDN2IN88US=> MYfTRW5ITVJ?
COR-L279 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkm1TWM2OD17LkO5NFkh|ryP MmXvV2FPT0WU
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BC-3 NIXqXYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH64ZYFKSzVyPUGyMlQ3PTFizszN Mnv0V2FPT0WU
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NCI-H128 M4f2fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHTTWJjUUN3ME2xN{4xPzJ|IN88US=> M{jDWXNCVkeHUh?=
NCI-H1694 NH24PINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTF|LkGxOFQh|ryP NIr3R5dUSU6JRWK=
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NCI-H1770 Mn[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33XO2lEPTB;MUSuOVM3QSEQvF2= NHP4SoFUSU6JRWK=
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COR-L88 NG\BSpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXJXpY{UUN3ME2xOk4xODF{IN88US=> NIPP[ItUSU6JRWK=
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KALS-1 NUG2TlJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVztNIZtUUN3ME2xOk42QTNzIN88US=> MXLTRW5ITVJ?
D-283MED NV3qeVA4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml2xTWM2OD1zNj64OFg6KM7:TR?= NHvITphUSU6JRWK=
NCI-H719 M3G2Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTF4LkmxOlEh|ryP M3v4[nNCVkeHUh?=
MLMA NXrmNJM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTlN4V[UUN3ME2xOk46QTB5IN88US=> NYfi[3lZW0GQR1XS
EVSA-T NF;NNIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TxRmlEPTB;MUeuNFQ5PSEQvF2= MVrTRW5ITVJ?
SK-N-FI MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPpTWM2OD1zNz62PVE{KM7:TR?= M4HuNXNCVkeHUh?=
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NCI-H1882 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlX4TWM2OD1zNz65PFM1KM7:TR?= Mn2wV2FPT0WU
A704 MkL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PLSGlEPTB;MUeuPVkxPCEQvF2= MoHXV2FPT0WU
L-428 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHe5empKSzVyPUG4MlAyPTFizszN NHzhT|JUSU6JRWK=
HCC1187 NYrDS5llT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17RNGlEPTB;MUiuNFE5PyEQvF2= M{Pve3NCVkeHUh?=
NCI-H1581 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPQRVJKSzVyPUG4MlA5PjZizszN MUjTRW5ITVJ?
BB65-RCC MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTF6LkSxOlIh|ryP NV\k[2xRW0GQR1XS
EM-2 NVTkXmF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo[2TWM2OD1zOD61OlczKM7:TR?= NEe3WnBUSU6JRWK=
Raji NGDFZ|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDvS3lKSzVyPUG5Mlk2PjVizszN NUTtcmtPW0GQR1XS
TE-1 NYLKUZh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrV[YpKSzVyPUKwMlQyODRizszN MVTTRW5ITVJ?
SW962 NX[w[G83T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1POfmlEPTB;MkCuOFI6OyEQvF2= NYe3eVJuW0GQR1XS
MHH-NB-11 NFrkVZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfxfWduUUN3ME2yNE42PTJzIN88US=> MXXTRW5ITVJ?
no-10 NUnh[ldiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTJzLkCyOlQh|ryP M33qc3NCVkeHUh?=
GDM-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEezXo1KSzVyPUKxMlk1OTRizszN NWS3XYwxW0GQR1XS
KMS-12-PE MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rjb2lEPTB;MkKuNlc1KM7:TR?= MXHTRW5ITVJ?
NCI-H510A NXHsdFNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\MTWM2OD1{ND6xNlc5KM7:TR?= NELaPFFUSU6JRWK=
ES5 MnO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DIXWlEPTB;MkSuO|M1QSEQvF2= MkjNV2FPT0WU
JiyoyeP-2003 M3jzbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTJ4LkK3OFIh|ryP NGrZNYhUSU6JRWK=
NMC-G1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXkTWM2OD1{Nz6xPFIzKM7:TR?= NGPhc5RUSU6JRWK=
NCI-H446 M1H0emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXxUHhKSzVyPUK3MlQ6PDZizszN MV3TRW5ITVJ?
NB7 M4rMeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnjTWM2OD1{Nz65NlI6KM7:TR?= NInNV2pUSU6JRWK=
A388 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;DUmlEPTB;MkiuNFA4PCEQvF2= MWfTRW5ITVJ?
JVM-2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTJ6LkK4PVgh|ryP NVfNVplyW0GQR1XS
HT-144 M3T0ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGD6Um9KSzVyPUK4MlY6KM7:TR?= MoXVV2FPT0WU
NCI-H747 MmWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjCPFFxUUN3ME2yPE46OTl3IN88US=> NFm5V41USU6JRWK=
NCI-H1650 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPZ[5lKSzVyPUK5MlAyPzZizszN MWTTRW5ITVJ?
EB-3 NG[zOXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\VTWM2OD1{OT61N|A6KM7:TR?= NWLXdWNZW0GQR1XS
KLE M3;Scmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HIZmlEPTB;MkmuOlE6KM7:TR?= NWTWeHBmW0GQR1XS
TK10 M4DYSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknzTWM2OD1|MD6xNlYh|ryP NUDW[5VWW0GQR1XS
COLO-668 MmOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfFNoZKSzVyPUOwMlc6OiEQvF2= NFTubVFUSU6JRWK=
NCI-H23 M2Xpe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Di[WlEPTB;M{GuNVA3OyEQvF2= NH;kWHVUSU6JRWK=
GOTO MnnGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTNzLk[wPFUh|ryP NFrEUZhUSU6JRWK=
MSTO-211H NED2SlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUn2TIEzUUN3ME2zNU45Pjd6IN88US=> NH3PPXVUSU6JRWK=
LB831-BLC MlLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPpTWM2OD1|Mj6zPFQ{KM7:TR?= MmnCV2FPT0WU
SCH M1nFPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn:zTWM2OD1|Mj64OFg2KM7:TR?= M2LTS3NCVkeHUh?=
EHEB M4fFeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\pPWlEPTB;M{SuNVE6OyEQvF2= M1rYTnNCVkeHUh?=
U-266 NULzO5BYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPvTWM2OD1|ND6yO|gyKM7:TR?= MkfNV2FPT0WU
EW-11 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfjTWM2OD1|ND60O|I2KM7:TR?= MlraV2FPT0WU
TE-9 NH23PWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\1dpdKSzVyPUO3MlA1ODFizszN NIDTNI9USU6JRWK=
ES3 NHjk[XFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DjPWlEPTB;M{euOVAxPCEQvF2= M1[yUnNCVkeHUh?=
NCI-H2141 NH\ZfnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnP5TWM2OD1|OD6wPFQ{KM7:TR?= MX\TRW5ITVJ?
MPP-89 M1GyOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Twe2lEPTB;NEKuNFU5PiEQvF2= NXLBd4lGW0GQR1XS
SK-MEL-2 MmrlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfLTWM2OD12Mj62OFA2KM7:TR?= NXPKR3dvW0GQR1XS
LC-1F MnH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTR|LkO2PFIh|ryP MV;TRW5ITVJ?
NH-12 MoXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;ZZ44yUUN3ME20N{46OzV7IN88US=> NGWxVlhUSU6JRWK=
RKO M2nIS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXW[JlKSzVyPUS0MlEzPTJizszN M3:yU3NCVkeHUh?=
KM-H2 NYnIb|JLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrwXZJKSzVyPUS0Mlk2PzdizszN NYX5d|ExW0GQR1XS
SK-UT-1 NYnMdXRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDjTWM2OD12OT64PFI2KM7:TR?= MlP0V2FPT0WU

... Click to View More Cell Line Experimental Data

In vivo Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. [2] Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model. [3]

Protocol

Kinase Assay:[1]
+ Expand

Biochemical Tyrosine Kinase Assays:

IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferasefusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST. The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate.
Cell Research:[3]
+ Expand
  • Cell lines: RS4;11, MV4;11, and OC1-AML5
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 24 and 48 hours
  • Method: Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Female nu/nu mice implanted s.c. with HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, and male nu/nu mice bearing luciferase-expressing PC-3M tumors
  • Formulation: Formulated as a carboxymethyl cellulose suspension or as a citrate buffered (pH 3.5) solution
  • Dosages: ~80 mg/kg
  • Administration: Orally once daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 15 mg/mL (28.16 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
2mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 532.56
Formula

C22H27FN4O2.C4H6O5

CAS No. 341031-54-7
Storage powder
Synonyms N/A

Bio Calculators

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02761057 Recruiting Recurrent Renal Cell Carcinoma|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer|Type 1 Papillary Renal Cell Carcinoma|Type 2 Papillary Renal Cell Carcinoma National Cancer Institute (NCI) April 2016 Phase 2
NCT02779283 Recruiting Untreated Adult Acute Myeloid Leukemia OHSU Knight Cancer Institute|National Cancer Institute (NCI) December 2015 Phase 1
NCT02626754 Enrolling by invitation Renal Cell Carcinoma vghtpe user|Taipei Veterans General Hospital, Taiwan August 2015 Phase 2
NCT02465060 Recruiting Advanced Malignant Neoplasm|Lymphoma|Recurrent Plasma Cell Myeloma|Recurrent Solid Neoplasm|Refractory Malignant Neoplasm|Refractory Plasma Cell Myeloma National Cancer Institute (NCI) August 2015 Phase 2
NCT01835158 Active, not recruiting Clear Cell Renal Cell Carcinoma|Metastatic Renal Cell Cancer|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer National Cancer Institute (NCI) July 2013 Phase 2
NCT01740154 Terminated Fatigue|Recurrent Renal Cell Cancer|Stage IV Renal Cell Cancer Case Comprehensive Cancer Center|National Cancer Institute (NCI) September 2012 --

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    I was wondering that the compound is in its cis or trans form?

  • Answer:

    S1042 Sunitinib Malate is Z form.

  • Question 2:

    What is the difference between Sunitinib Malate(S1042) and Sunitinib(S7781)?

  • Answer:

    S1042 is the Malate salt form of Sunitinib. The biological activities of these two compounds are the same but the solubility of these two compounds in aqueous solvent are different.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID